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Submit ReviewNiclosamide is an inhibitor of the STAT3 signaling pathway; inhibits the activation, nuclear translocation and transactivation of STAT3. Niclosamide displays selectivity for STAT3 over STAT1, STAT5, JAK1, JAK2 and Src kinases. It inhibits the transcription of STAT3 target genes and induces cell growth inhibition, apoptosis and cell cycle arrest of cancer cells with constitutively active STAT3. It also reversibly inhibits mTORC1 signaling and stimulates autophagy in vitro; displays antineoplastic effects in acute myelogenous leukemia (AML) stem cells. In addition, niclosamide inhibits SARS-CoV-2 replication in vitro (IC50 = 0.34 μM in Vero E6 plaque assay) through suppression of TMEM16F activity.
分子量 | 325.99 |
公式 | C13H8Cl2N2O4 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 50-65-7 |
PubChem ID | 4477 |
InChI Key | RJMUSRYZPJIFPJ-UHFFFAOYSA-N |
Smiles | O=C(NC2=C(Cl)C=C([N+]([O-])=O)C=C2)C1=C(O)C=CC(Cl)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
ethanol | 8.15 | 25 | |
DMSO | 3.26 | 10 |
以下数据基于产品分子量 325.99。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.25 mM | 12.27 mL | 61.35 mL | 122.7 mL |
1.25 mM | 2.45 mL | 12.27 mL | 24.54 mL |
2.5 mM | 1.23 mL | 6.14 mL | 12.27 mL |
12.5 mM | 0.25 mL | 1.23 mL | 2.45 mL |
参考文献是支持产品生物活性的出版物。
Balgi et al (2009) Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLoS One 4 e7124 PMID: 19771169
Jin et al (2010) Antineoplastic mechanisms of niclosamide in acute myelogenous leukemia stem cells: inactivation of the NF-κB pathway and generation of reactive oxygen species. Cancer Res. 70 2516 PMID: 20215516
Ren et al (2010) Identification of niclosamide as a new small-molecule inhibitor of the STAT3 signaling pathway. ACS Med.Chem.Lett. 1 454 PMID: 24900231
Braga et al (2021) Drugs that inhibit TMEM16 proteins block SARS-CoV-2 spike-induced syncytia. Nature 594 88 PMID: 33827113
If you know of a relevant reference for Niclosamide, please let us know.
关键词: Niclosamide, Niclosamide supplier, STAT3, mTORC1, signaling, signalling, pathway, inhibitors, inhibits, anthelmintic, SARS-CoV-2, spike, TMEM16F, STAT, mTOR, Stem, Cell, Signaling, Autophagy, Cancer, Cells, Coronavirus, Ca2+-Activated, Chloride, Channels, 4079, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Niclosamide 的部分引用包括:
Eun-Kyoung et al (2017) The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. Int J Mol Sci 18 PMID: 29077055
Natarajan et al (2014) STAT3 modulation to enhance motor neuron differentiation in human neural stem cells. PLoS One 9 e100405 PMID: 24945434
Ru-Rong et al (2020) Periostin Activation of Integrin Receptors on Sensory Neurons Induces Allergic Itch. Cell Rep 31 107472 PMID: 32268102
Yan et al (2021) A Novel Biological Activity of the STAT3 Inhibitor Stattic in Inhibiting Glutathione Reductase and Suppressing the Tumorigenicity of Human Cervical Cancer Cells via a ROS-Dependent Pathway. Onco Targets Ther 14 4047-4060 PMID: 34262291
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